Example Data Sheet: Sirolimus

Description

Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 (Edwards and Wandless 2007). Rapamycin is an autophagy activator, an immunosuppressant (Rangaraju et al. 2010).

MOA

MTOR inhibitor
ITP

Drug Targets

FGF2
FKBP1A
MTOR (drug-ligand rendering)

Reactome Pathway

R-HSA-449147:Signaling by Interleukins
R-HSA-5663202:Diseases of signal transduction by growth factor receptors and second messengers
R-HSA-9006925:Intracellular signaling by second messengers
R-HSA-1257604:PIP3 activates AKT signaling
R-HSA-3700989:Transcriptional Regulation by TP53
R-HSA-6785807:Interleukin-4 and Interleukin-13 signaling
R-HSA-5633007:Regulation of TP53 Activity
R-HSA-9612973:Autophagy
R-HSA-1632852:Macroautophagy
R-HSA-6807070:PTEN Regulation

Signaling by Interleukins

Signaling by Interleukins

Diseases of signal transduction by growth factor receptors and second messengers

Diseases of signal transduction by growth factor receptors and second messengers

Intracellular signaling by second messengers

Intracellular signaling by second messengers

PIP3 activates AKT signaling

PIP3 activates AKT signaling

Transcriptional Regulation by TP53

Transcriptional Regulation by TP53

Interleukin-4 and Interleukin-13 signaling

Interleukin-4 and Interleukin-13 signaling

Regulation of TP53 Activity

Regulation of TP53 Activity

Autophagy

Autophagy

Macroautophagy

Macroautophagy

PTEN Regulation

PTEN Regulation

References

Edwards, Sarah R., and Thomas J. Wandless. 2007. “The Rapamycin-Binding Domain of the Protein Kinase Mammalian Target of Rapamycin Is a Destabilizing Domain.” Journal of Biological Chemistry 282 (18): 13395–401. https://doi.org/10.1074/jbc.m700498200.
Rangaraju, Sunitha, Jonathan D. Verrier, Irina Madorsky, Jessica Nicks, William A. Dunn, and Lucia Notterpek. 2010. “Rapamycin Activates Autophagy and Improves Myelination in Explant Cultures from Neuropathic Mice.” The Journal of Neuroscience 30 (34): 11388–97. https://doi.org/10.1523/jneurosci.1356-10.2010.